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Dazdotuftide
Tier C · 观察 / 贸易Dazdotuftide
Tarsius Pharma
原研
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首批上市
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到期年(公开口径)
无销量数据
峰值销售
小分子
类型
靶点:NF-κB
适应症(已批准):葡萄膜炎、前葡萄膜炎、青光眼、眼睛发炎
各地区研发/上市状态
美国
临床三期
2021-09-20
欧盟
临床三期
2021-09-20
中国
-
日本
-
合成路线与中间体2 routes
原研路线 × 0优化路线(非专利)× 2工艺路线 × 0
路线按「原研路线 → 优化路线 / 工艺路线(非专利)」排序。每条路线附本站自绘的路线流程图(中间体 → 原料药)与中间体表(编号 / CAS / 英文名),可直接用于供应商开发与询价。流程图由本站依据已授权的结构化数据自行渲染,未使用任何第三方路线图。
优化Route 1步骤 5 · 总收率 /
(I)1062329-1-a—(II)1062329-1-a—(IIIb)1062329-1-a3978-80-1(IVa)1062329-1-a—(IVb)1062329-1-a—(V)1062329-1-a—(VIa)1062329-1-a29022-11-5(VIb)1062329-1-a4530-20-5(VII)1062329-1-a—(VIIIa)1062329-1-a154445-77-9(VIIIb)1062329-1-a200124-22-7(IX)1062329-1-a,(IX)1062329-1-b—API · Dazdotuftide
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1062329-1-a | - | 4-Aminophenyl 2-(trimethylammonio)ethyl phosphate |
| (II)1062329-1-a | - | 4-Diazoniophenyl 2-(trimethylazaniumyl)ethyl phosphate chloride |
| (IIIb)1062329-1-a | 3978-80-1 | (2S)-3-(4-Hydroxyphenyl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoic acid |
| (IVa)1062329-1-a | - | N-[[(9H-Fluoren-9-yl)methoxy]carbonyl]-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]-L-tyrosine |
| (IVb)1062329-1-a | - | N-(tert-Butoxycarbonyl)-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]-L-tyrosine |
| (V)1062329-1-a | - | Resin bound 3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]-L-tyrosine |
| (VIa)1062329-1-a | 29022-11-5 | 2-(9H-Fluoren-9-ylmethoxycarbonylamino)acetic acid |
| (VIb)1062329-1-a | 4530-20-5在售 | 2-((tert-Butoxycarbonyl)amino)acetic acid |
| (VII)1062329-1-a | - | Resin bound glycyl-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]-L-tyrosine |
| (VIIIa)1062329-1-a | 154445-77-9 | (2S)-2-{[(9H-Fluoren-9-ylmethoxy)carbonyl]amino}-5-[2-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]pentanoic acid |
| (VIIIb)1062329-1-a | 200124-22-7 | (2S)-2-{[(tert-Butoxy)carbonyl]amino}-5-{N'-[(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-yl)sulfonyl]carbamimidamido}pentanoic acid |
| (IX)1062329-1-a,(IX)1062329-1-b | - | Resin bound N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithylglycyl-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]-L-tyrosine |
优化Route 2步骤 4 · 总收率 /
(IX)1062329-1-a,(IX)1062329-1-b—(Xa)1062329-1-b71989-31-6(Xb)1062329-1-b15761-39-4(XI)1062329-1-b—(XIIa)1062329-1-b71989-26-9(XIIb)1062329-1-b2483-46-7(XIII)1062329-1-b—(XIVa)1062329-1-b71989-35-0(XIVb)1062329-1-b13734-40-2(XV)1062329-1-b—(XVI)1062329-1-b—API · Dazdotuftide
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (IX)1062329-1-a,(IX)1062329-1-b | - | Resin bound N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithylglycyl-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]-L-tyrosine |
| (Xa)1062329-1-b | 71989-31-6 | (2S)-1-{[(9H-Fluoren-9-yl)methoxy]carbonyl}pyrrolidine-2-carboxylic acid |
| (Xb)1062329-1-b | 15761-39-4 | (2S)-1-[(2-Methylpropan-2-yl)oxycarbonyl]pyrrolidine-2-carboxylic acid |
| (XI)1062329-1-b | - | Resin bound [(2S)-3-(4-hydroxy-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]phenyl)-2-([L-prolyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithylglycyl]amino)propanoyl]oxy |
| (XIIa)1062329-1-b | 71989-26-9 | (2S)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-6-[(2-methylpropan-2-yl)oxycarbonylamino]hexanoic acid |
| (XIIb)1062329-1-b | 2483-46-7 | (2S)-2,6-Bis({[(tert-butoxy)carbonyl]amino})hexanoic acid |
| (XIII)1062329-1-b | - | Resin bound [(2S)-2-([N6-(tert-butoxycarbonyl)-L-lysyl-L-prolyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithylglycyl]amino)-3-(4-hydroxy-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]phenyl)propanoyl]oxy |
| (XIVa)1062329-1-b | 71989-35-0 | O-tert-Butyl-N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-threonine |
| (XIVb)1062329-1-b | 13734-40-2 | N-(tert-Butoxycarbonyl)-O-tert-butyl-L-threonine |
| (XV)1062329-1-b | - | Resin bound [(2S)-2-([O-tert-butyl-L-threonyl-N6-(tert-butoxycarbonyl)-L-lysyl-L-prolyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithylglycyl]amino)-3-(4-hydroxy-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]phenyl)propanoyl]oxy |
| (XVI)1062329-1-b | - | L-Threonyl-L-lysyl-L-prolyl-L-arginylglycyl-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]-L-tyrosine--trifluoroacetic acid (1/1) |
常见问题(FAQ)
Dazdotuftide的适应症有哪些?
已批准的适应症包括:葡萄膜炎、前葡萄膜炎、青光眼、眼睛发炎。
Dazdotuftide的专利什么时候到期?
Dazdotuftide的专利到期年暂无公开口径,本页会在数据管道核实后更新。
Dazdotuftide有几条合成路线?
本站收录 2 条合成路线,最短路线 4 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
Dazdotuftide的关键中间体在哪里可以采购?
Dazdotuftide的多条路线中间体已挂接 CAS 档案,其中 1 个 CAS 已有优贝德(Unibest)供应网络在售报价,可在本页路线表中直接查看并询价。
如何获取Dazdotuftide中间体的报价?
在本页选择目标中间体的 CAS 进入档案页,或在询价页直接提交需求;CAS 会自动带入供需撮合流程,由供应网络反馈报价。
数据来源:多源数据交叉核实(仅结构化字段) · 2026-10-21